US11273133B2ActiveUtilityA1

Bupropion as a modulator of drug activity

99
Assignee: ANTECIP BIOVENTURES II LLCPriority: Nov 5, 2013Filed: Jan 11, 2019Granted: Mar 15, 2022
Est. expiryNov 5, 2033(~7.3 yrs left)· nominal 20-yr term from priority
Inventors:Herriot Tabuteau
A61K 31/137A61K 31/138A61K 31/485A61K 2300/00
99
PatentIndex Score
65
Cited by
500
References
30
Claims

Abstract

Dosage forms, drug delivery systems, methods related to sustained release of dextromethorphan or improved therapeutic effects. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A method of increasing dextromethorphan plasma levels in a human being comprising administering for at least eight consecutive days a combination of dextromethorphan and bupropion to a human being, wherein the bupropion and the dextromethorphan are co-administered in a dosage form containing bupropion and dextromethorphan as the only active pharmaceutical agents, wherein the human being is a non-poor metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the combination is administered twice a day for at least eight consecutive days, wherein the treatment has a therapeutic effect, and wherein the combination is administered in a dosage form having properties effective for providing a Cmax of dextromethorphan on the eighth day of at least about 50 ng/mL, and wherein on the eighth day the combination is administered the Cmax of dextromethorphan is at least about 20 times the Cmax of dextromethorphan that would be achieved by administering the same amount of the dextromethorphan without the bupropion for eight consecutive days. 
     
     
       2. The method of  claim 1 , wherein the dosage form is a single oral dosage form. 
     
     
       3. The method of  claim 2 , wherein the single oral dosage form is a solid. 
     
     
       4. The method of  claim 3 , wherein the single solid oral dosage form further comprises a binder, a disintegrating agent or a lubricant. 
     
     
       5. The method of  claim 3 , wherein the single solid oral dosage form is a tablet, a troche, a pill, or a capsule. 
     
     
       6. The method of  claim 2 , wherein the single oral dosage form is a liquid. 
     
     
       7. The method of  claim 6 , wherein the single liquid dosage form comprises a liquid or a solid phase dispersion of bupropion and dextromethorphan. 
     
     
       8. The method of  claim 1 , wherein the dosage form is effective for immediate release of dextromethorphan. 
     
     
       9. The method of  claim 1 , wherein the dosage form is effective for sustained release of bupropion. 
     
     
       10. The method of  claim 1 , wherein the C max  of dextromethorphan on the eighth day is at least about 60 ng/mL. 
     
     
       11. The method of  claim 1 , wherein the C max  of dextromethorphan on the eighth day is at least about 70 ng/mL. 
     
     
       12. The method of  claim 1 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the combination is administered is at least about 600 ng·hr/mL. 
     
     
       13. The method of  claim 1 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the combination is administered is at least about 700 ng·hr/mL. 
     
     
       14. The method of  claim 1 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the combination is administered is about 500 ng·hr/mL to about 600 ng·hr/mL. 
     
     
       15. The method of  claim 1 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the combination is administered is about 550 ng·hr/mL to about 600 ng·hr/mL. 
     
     
       16. A method for treating a human being with dextromethorphan by increasing dextromethorphan plasma levels comprising administering dextromethorphan and bupropion twice daily for at least eight consecutive days, wherein the bupropion and the dextromethorphan are co-administered in a dosage form containing bupropion and dextromethorphan as the only active pharmaceutical agents, wherein the human being is a non-poor metabolizer of dextromethorphan in need of treatment with dextromethorphan, wherein the treatment has a therapeutic effect, and wherein dextromethorphan and bupropion are administered in amounts that result in an AUC 0-12  of dextromethorphan on the eighth day that dextromethorphan and bupropion are administered that is at least about 500 ng·hr/mL, and wherein the AUC 0-12  of dextromethorphan on the eighth day that the dextromethorphan and the bupropion are administered is at least about 30 times the AUC 0-12  of dextromethorphan that would result from administering the same amount of the dextromethorphan without the bupropion. 
     
     
       17. The method of  claim 16 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the dextromethorphan and the bupropion are administered is at least about 600 ng·hr/mL. 
     
     
       18. The method of  claim 16 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the dextromethorphan and the bupropion are administered is at least about 700 ng·hr/mL. 
     
     
       19. The method of  claim 16 , wherein the AUC 0-12  of dextromethorphan on the eighth day that the dextromethorphan and the bupropion are administered is at least about 800 ng·hr/mL. 
     
     
       20. The method of  claim 16 , wherein the C max  of dextromethorphan on the eighth day is at least about 60 ng/mL. 
     
     
       21. The method of  claim 16 , wherein the C max  of dextromethorphan on the eighth day is at least about 70 ng/mL. 
     
     
       22. The method of  claim 16 , wherein the bupropion and the dextromethorphan are co-administered together in a single oral dosage form. 
     
     
       23. The method of  claim 22 , wherein the single oral dosage form is a solid. 
     
     
       24. The method of  claim 23 , wherein the single solid oral dosage form further comprises a binder, a disintegrating agent, or a lubricant. 
     
     
       25. The method of  claim 23 , wherein the single solid oral dosage form is a tablet, a troche, a pill, or a capsule. 
     
     
       26. The method of  claim 22 , wherein the single oral dosage form is a liquid. 
     
     
       27. The method of  claim 26 , wherein the single liquid dosage form comprises a liquid or a solid phase dispersion of bupropion and dextromethorphan. 
     
     
       28. The method of  claim 22 , wherein the single oral dosage form is effective for immediate release of dextromethorphan. 
     
     
       29. The method of  claim 22 , wherein the single oral dosage form is effective for sustained release of bupropion. 
     
     
       30. The method of  claim 16 , wherein the co-administration is effective for increasing dextromethorphan plasma levels in the human being.

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